Pharmacology Part 1 Flashcards
Define pharmacodynamics?
What a drug does to the body (biological effects and mechanisms of action)
Define pharmacokinetics?
What the body does to a drug (absorption, distribution, metabolism and excretion of drugs and their metabolites)
What is the narrow definition of a drug?
Any single use synthetic, or natural,, substance of known structure used in the treatment, prevention, or diagnosis of a disease
Define a medicine
A chemical preparation containing one or more drugs used with the intention of causing a therapeutic effect.
What must a drug be in order to be a useful therapeutic agent?
Selective
What does drug selectivity result from?
The chemical structure of the drug (binding site)
The target containing only ligands of a precise structure (ligand specificity)
What regulatory proteins do drugs bind to?
Enzymes
Carrier molecules (transporters and pumps)
Ion channels
Receptors
What non-regulatory proteins can drugs bind to?
RNA
DNA
Define a receptor
Macromolecules that mediate the biological actions of hormones and neurotransmitters
Define an agonist drug
Binds to receptor to produce a cellular response
Define an antagonist drug
Blocks the actions of an agonist by binding to the same receptor
Describe the action of adrenaline
Binds to receptors (B-adrenoreceptors) in the heart to increase cardiac rate. It is an agonist.
Describe the action of B-blockers
Class of synthetic drug that bind to B-adrenoreceptors in the heart to block the binding of adrenaline- they are antagonists and prevent the increase in cardiac rate and force
What do agonists possess?
Affinity and Efficacy
Define agonist affinity?
The strength of association between a ligand and receptor determined by chemical bonds
Define agonist efficacy?
The ability of an agonist to evoke a cellular response
What do agonists and antagonists do when they bind to receptors?
Agonists: Activate
Antagonists: bind
What do antagonists possess?
Affinity but lack efficacy
Describe the relationship of concentration (or dose) and response
It is hyperbolic
What is EC50
The concentration of agonist that elicits half maximal response
Describe the relationship between agonist concentration (or dose) and response on a semi-logarithmic plot?
Sigmoidal
What is potency?
The concentration of a drug required to achieve a response
How does competitive antagonism occur?
When the binding of the agonist and antagonist occur at the same (orthosteric) site
When does non-competitive antagonism occur?
When the agonist binds to the orthosteric site and antagonist binds to the allosteric site, so both may bind simultaneously but activation cannot occur when the antagonist is bound
What do competitive antagonist do to the response curve?
Cause a parallel rightward shift of the agonist concentration response curve with no depression of the maximal response.
What do non-competitive antagonists do to the response curve?
Depress the slope and the maximum response response of the curve. Do not cause a rightward shift.